1672665-49-4

1672665-49-4 structure

Name: PT-2385
Chemical Name: PT2385
CAS Number: 1672665-49-4
Molecular Formula: C₁₇H₁₂F₃NO₄S
Molecular Weight: 383.342
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIF/HIF Prolyl-Hydroxylase
Create Date: 2018-05-21 08:00:00
Modify Date: 2024-01-10 04:53:52
PT-2385 is a selective HIF-2α antagonist with a Ki of less than 50 nM.

Name	PT2385
Synonyms	Benzonitrile, 3-[[(1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro- 3-{[(1S)-2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl]oxy}-5-fluorobenzonitrile PT-2385

Description	PT-2385 is a selective HIF-2α antagonist with a Ki of less than 50 nM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase Research Areas >> Cancer
Target	Kd: <50 nM (HIF-2α)[1]
In Vitro	PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α[1].
In Vivo	PT-2385 (PT2385) inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT-2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT-2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT-2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31)[1].
References	[1]. Eli Wallace, Ph.D. PT2385: HIF-2α Antagonist for the Treatment of VHL Mutant ccRCC. 12th International VHL Medical Symposium April 8, 2016. [2]. Xie C, et al. Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis. Nat Med. 2017 Nov;23(11):1298-1308.